CA3143471C - Formulation a longue duree d'action contenant de la rivastigmine et son procede de preparation - Google Patents

Formulation a longue duree d'action contenant de la rivastigmine et son procede de preparation Download PDF

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Publication number
CA3143471C
CA3143471C CA3143471A CA3143471A CA3143471C CA 3143471 C CA3143471 C CA 3143471C CA 3143471 A CA3143471 A CA 3143471A CA 3143471 A CA3143471 A CA 3143471A CA 3143471 C CA3143471 C CA 3143471C
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CA
Canada
Prior art keywords
microsphere
rivastigmine
acid
sustained release
sample
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Active
Application number
CA3143471A
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English (en)
Other versions
CA3143471A1 (fr
Inventor
Heeyong Lee
Eunyoung SEOL
Juhan Lee
Yeonkyeong Lee
Donghyun Park
Heekyoung CHOE
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G2gbio Inc
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G2gbio Inc
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Publication of CA3143471A1 publication Critical patent/CA3143471A1/fr
Application granted granted Critical
Publication of CA3143471C publication Critical patent/CA3143471C/fr
Active legal-status Critical Current
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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions

Abstract

La présente invention concerne : des microsphères à libération prolongée pour une formulation injectable contenant un polymère biodégradable et au moins un principe actif choisi dans le groupe constitué de la rivastigmine et de ses sels de qualité pharmaceutique peu solubles ; une formulation injectable à longue durée d'action qui est destinée à prévenir ou traiter la maladie d'Alzheimer et qui contient les microsphères ; et un procédé de préparation des microsphères. La présente invention concerne une formulation injectable à longue durée d'action contenant des microsphères de rivastigmine à libération prolongée, dans lesquelles une libération initiale rapide du médicament est efficacement régulée même si la teneur en médicament est élevée, et qui peut ainsi maximiser les effets thérapeutiques en réduisant les effets secondaires associés au tractus gastro-intestinal et qui se produisent souvent chez les patients qui reçoivent des médicaments classiques administrés par voie orale, avec pour conséquence un renforcement de l'observance thérapeutique.
CA3143471A 2019-07-12 2020-07-13 Formulation a longue duree d'action contenant de la rivastigmine et son procede de preparation Active CA3143471C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR20190084775 2019-07-12
KR10-2019-0084775 2019-07-12
PCT/KR2020/009221 WO2021010719A1 (fr) 2019-07-12 2020-07-13 Formulation à longue durée d'action contenant de la rivastigmine et son procédé de préparation

Publications (2)

Publication Number Publication Date
CA3143471A1 CA3143471A1 (fr) 2021-01-21
CA3143471C true CA3143471C (fr) 2023-10-31

Family

ID=74211043

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3143471A Active CA3143471C (fr) 2019-07-12 2020-07-13 Formulation a longue duree d'action contenant de la rivastigmine et son procede de preparation

Country Status (11)

Country Link
US (1) US20220257518A1 (fr)
EP (1) EP3998065A4 (fr)
JP (2) JP7437074B2 (fr)
KR (4) KR20210007924A (fr)
CN (1) CN114126592A (fr)
AU (1) AU2020312361A1 (fr)
BR (1) BR112022000413A2 (fr)
CA (1) CA3143471C (fr)
MX (1) MX2022000489A (fr)
WO (1) WO2021010719A1 (fr)
ZA (1) ZA202201465B (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210158232A (ko) * 2020-06-23 2021-12-30 주식회사 아울바이오 치매치료를 위한 장기지속형 주사제
CN115124456A (zh) * 2021-03-26 2022-09-30 上海博志研新药物技术有限公司 哌马色林药用盐、制备方法、含其的药物组合物及应用
CN113877000B (zh) * 2021-10-13 2023-01-24 科笛生物医药(无锡)有限公司 注射用微球组合物及其应用
WO2023249465A1 (fr) * 2022-06-23 2023-12-28 주식회사 지투지바이오 Formulation de microsphères à action prolongée contenant de l'entécavir, et son procédé de préparation
KR20240000405A (ko) * 2022-06-23 2024-01-02 주식회사 지투지바이오 약물과 파모산을 함유하는 서방성 미립구

Family Cites Families (11)

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KR100333115B1 (ko) * 1992-11-17 2002-12-02 미츠비시 파마 코포레이션 항정신병약함유서방성마이크로스피어및이의제조방법
MY148370A (en) * 2006-12-18 2013-04-15 Takeda Pharmaceutical Sustained-release composition and method for producing the same
CN101708164A (zh) 2009-12-18 2010-05-19 苏州大学 一种卡巴拉汀缓释微球及其制备方法
KR20120011344A (ko) * 2010-07-21 2012-02-08 에스케이케미칼주식회사 고분자 미립구의 제조방법 및 그 방법에 의해 제조된 고분자 미립구
KR101424163B1 (ko) * 2010-12-24 2014-08-01 주식회사 삼양바이오팜 수난용성 약물 함유 서방성 마이크로입자 및 그 제조방법
WO2013078608A1 (fr) * 2011-11-29 2013-06-06 Ziqiang Gu Pamoate de donepezil et ses procédés de fabrication et d'utilisation
KR101307729B1 (ko) * 2012-11-19 2013-09-11 에스케이케미칼주식회사 초기 약물 방출이 감소된 고분자 미립자를 포함하는 주사용 조성물 및 이의 제조방법
KR101811797B1 (ko) * 2013-04-03 2017-12-22 동국제약 주식회사 도네페질을 포함하는 비경구투여용 약제학적 조성물
KR101961848B1 (ko) * 2016-08-25 2019-03-25 영진약품 주식회사 C18:1, c18:1(oh) 또는 c18:2의 장쇄 지방산이 포함된 오일류를 포함한 방출억제제를 적용한 서방출성 마이크로스피어 및 이의 제조방법
KR101900482B1 (ko) * 2017-01-17 2018-09-19 한국화학연구원 미립구형 서방출 주사제 및 그의 제조방법
KR102047983B1 (ko) * 2017-11-30 2019-11-22 주식회사 지투지바이오 안전성 및 저장 안정성이 향상된 생분해성 미립구의 제조방법

Also Published As

Publication number Publication date
KR20210007924A (ko) 2021-01-20
BR112022000413A2 (pt) 2022-03-03
WO2021010719A1 (fr) 2021-01-21
CA3143471A1 (fr) 2021-01-21
KR20210065921A (ko) 2021-06-04
CN114126592A (zh) 2022-03-01
JP7437074B2 (ja) 2024-02-22
KR20220044921A (ko) 2022-04-12
JP2024010233A (ja) 2024-01-23
ZA202201465B (en) 2023-11-29
EP3998065A4 (fr) 2023-07-12
AU2020312361A1 (en) 2022-03-03
MX2022000489A (es) 2022-02-03
US20220257518A1 (en) 2022-08-18
KR20220112737A (ko) 2022-08-11
EP3998065A1 (fr) 2022-05-18
JP2022541011A (ja) 2022-09-21

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